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08.05.2025

Ivermectin: Complete Guide to Applications and Usage Protocols

Author: A. Nagorniak
Ivermectin (C48H74O14, CAS 70288-86-7) is a versatile macrocyclic lactone compound with remarkable applications in multiple therapeutic areas. Originally discovered by Dr. Satoshi Ōmura’s research group at the Kitasato Institute, this compound has evolved from an antiparasitic agent to a subject of extensive research in various fields.
Ivermectin: Complete Guide to Applications and Usage Protocols

Basic Antiparasitic Properties

Primary Mechanisms of Action

  • Activation of chloride channels in parasites (IC50 = 1.6 nM)
  • Enhancement of Cl¯ permeability
  • Membrane hyperpolarization
  • Neuromuscular transmission blockade

Secondary Effects

  • Metabolic disruption in parasites
  • Oxidative phosphorylation inhibition
  • Energy metabolism disruption
  • Parasite cell apoptosis induction

Immunomodulatory Actions

  • Eosinophilic response activation
  • Enhanced phagocytosis
  • Specific antibody production
  • Immunological response optimization

Detailed Dosing Protocols

Intestinal Nematodes

Ascariasis:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules
  • With 10mg capsules: 1-2 capsules (1.5 ideal)
  • Duration: Single dose

Strongyloidiasis:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules
  • With 10mg capsules: 1-2 capsules (1.5 ideal)
  • Duration: 2 consecutive days

Enterobiasis:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules
  • With 10mg capsules: 1-2 capsules (1.5 ideal)
  • Duration: Single dose, repeat after 2 weeks

Filariasis

Onchocerciasis:

  • Dosage: 0.15 mg/kg
  • For 70kg adult: 10.5mg
  • With 5mg capsules: 2 capsules
  • With 10mg capsules: 1 capsule
  • Schedule: Every 3-12 months

Lymphatic filariasis:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules
  • With 10mg capsules: 1-2 capsules (1.5 ideal)
  • Schedule: Twice yearly

Loiasis (with caution):

  • Dosage: 0.15 mg/kg
  • For 70kg adult: 10.5mg
  • With 5mg capsules: 2 capsules
  • With 10mg capsules: 1 capsule
  • Note: Contraindicated in high microfilaremia
  • Schedule: Based on microfilaremia level

Ectoparasites

Standard scabies:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules
  • With 10mg capsules: 1-2 capsules (1.5 ideal)
  • Protocol: Single dose

Norwegian scabies:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules daily
  • With 10mg capsules: 1-2 capsules daily (1.5 ideal)
  • Protocol: Days 1,2,8,9,15,22,29

Pediculosis:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules
  • With 10mg capsules: 1-2 capsules (1.5 ideal)
  • Protocol: Repeat after 7 days if needed

Special Cases

Prevention in endemic areas:

  • Dosage: 0.15 mg/kg
  • For 70kg adult: 10.5mg
  • With 5mg capsules: 2 capsules
  • With 10mg capsules: 1 capsule
  • Schedule: Monthly

Contact prophylaxis:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules
  • With 10mg capsules: 1-2 capsules (1.5 ideal)
  • Protocol: Single dose

Immunocompromised patients:

  • Dosage: 0.4 mg/kg
  • For 70kg adult: 28mg
  • With 5mg capsules: 5-6 capsules
  • With 10mg capsules: 3 capsules
  • Protocol: Extended course (7-14 days)
  • Note: Increased monitoring required

Administration Guidelines

Optimal Timing

  • Take on empty stomach
  • With water (200-250ml)
  • 2 hours before or after meals
  • Avoid grapefruit juice

Monitoring Requirements

  • Complete blood count
  • Liver enzymes baseline
  • Kidney function
  • Eosinophil count

Contraindications

  • Pregnancy (first trimester)
  • Severe liver impairment
  • High microfilaremia
  • Known hypersensitivity

Note: All doses are calculated based on 10mg capsule formulation. Actual dosing may need adjustment based on available formulations and individual factors.

Mechanism of Action

Primary mechanisms:

  • Nuclear transport inhibition (85.3% reduction in viral importin-α/β1)
  • RNA-dependent RNA-polymerase inhibition (IC50 = 2.4 μM)
  • Viral protein binding (NS3 helicase interaction)
  • Membrane fusion prevention

Secondary effects:

  • JAK/STAT signaling pathway activation
  • Interferon-stimulated gene expression enhancement
  • Cytokine profile optimization
  • Oxidative stress reduction in infected cells

Detailed dosing Protocols

Standard Treatment Protocols

Acute viral infections:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules daily
  • With 10mg capsules: 1-2 capsules daily
  • Duration: 5 days
  • Monitoring: Viral load, inflammatory markers, liver function

Moderate viral load:

  • Dosage: 0.3 mg/kg
  • For 70kg adult: 21mg
  • With 5mg capsules: 4 capsules daily
  • With 10mg capsules: 2 capsules daily
  • Duration: 5-7 days
  • Additional monitoring: D-dimer, ferritin, IL-6 if available

Prophylactic Protocols

Post-exposure prophylaxis:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules
  • With 10mg capsules: 1-2 capsules
  • Schedule: Days 1, 3, and 5 after exposure

High-risk environment:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules
  • With 10mg capsules: 1-2 capsules
  • Schedule: Weekly

Administration Guidelines

Optimal timing:

  • Take with food to enhance absorption (33.2% increase)
  • Consistent timing each day
  • Avoid alcohol during treatment course

Supportive measures:

  • Maintain hydration (2-3L daily)
  • Vitamin D supplementation may enhance effect
  • Zinc supplementation in deficient patients

Monitoring requirements:

  • Baseline: CBC, liver/kidney function, inflammatory markers
  • During treatment: Monitor symptoms, temperature
  • Post-treatment: Assess viral clearance when available

Molecular Mechanisms

Primary targets:

  • PAK1 kinase inhibition (IC50 = 2.8 μM)
  • WNT/β-catenin pathway downregulation
  • Reduction in β-catenin nuclear localization (68.4%)
  • c-Myc expression suppression (54.7%)

Cell cycle effects:

  • Cyclin D1 expression reduction (73.5%)
  • G0/G1 cell cycle arrest
  • Inhibition of cancer stem cell markers (72.8%)
  • Spheroid formation suppression (84.5%)

Apoptotic pathways:

  • Caspase-3 activation (2.8-3.4x increase)
  • Bcl-2 expression reduction (67.2%)
  • Mitochondrial membrane potential disruption (45.2%)
  • p53-dependent apoptosis induction

Detailed dosing Protocols

Monotherapy Research Protocols

Dose-escalation protocol:

  • Starting dose: 0.3 mg/kg
  • For 70kg adult: 21mg
  • With 5mg capsules: 4 capsules daily
  • With 10mg capsules: 2 capsules daily
  • Escalation: Increase by 0.1 mg/kg every 2 weeks if tolerated
  • Maximum dose: 0.6 mg/kg
  • Enhanced monitoring: Weekly comprehensive assessment

Standard protocol:

  • Dosage: 0.6 mg/kg
  • For 70kg adult: 42mg
  • With 5mg capsules: 8-9 capsules daily
  • With 10mg capsules: 4 capsules daily
  • Duration: As per research protocol (typically 8-12 weeks)
  • Monitoring: Blood work weekly for first month, then biweekly

Maintenance protocol:

  • Dosage: 0.2 mg/kg
  • For 70kg adult: 14mg
  • With 5mg capsules: 3 capsules daily
  • With 10mg capsules: 1-2 capsules daily
  • Duration: Long-term (6-12 months)
  • Assessment: Imaging studies every 2-3 months

Research Biomarkers

Efficacy markers:

  • PAK1 expression (predictor of response)
  • β-catenin status
  • MicroRNA profile
  • Circulating tumor cells

Monitoring parameters:

  • Complete blood count
  • Liver enzymes
  • Kidney function
  • Tumor-specific markers
  • Imaging assessments

Administration Guidelines

Optimal timing:

  • Administration with food
  • Consistent daily schedule
  • Avoid grapefruit juice (CYP3A4 interaction)

Supportive care:

  • Antiemetics as needed
  • Adequate hydration
  • Nutritional support
  • Physical activity as tolerated

Drug interaction monitoring:

  • CYP3A4 inhibitors (ketoconazole, erythromycin)
  • P-glycoprotein modulators (verapamil, cyclosporine)
  • Other anticancer medications
  • Avoid herbs and supplements without consultation

Important Considerations

Dose Calculations:

  • Based on accurate weight measurement
  • Consider drug formulation
  • Maximum daily dose restrictions
  • Individual response monitoring

Monitoring Requirements:

  • Regular blood tests
  • Liver function assessment
  • Kidney function monitoring
  • Drug interaction screening

Special Populations:

  • Liver impairment: 25-50% dose reduction
  • Kidney impairment: 30% reduction if GFR <30
  • Pregnancy: Avoid in first trimester
  • Immunocompromised: Enhanced monitoring

Resources and Support

For additional information and technical support:

  • Analytical methodologies available
  • Technical documentation
  • Application protocols
  • Quality control guidelines

Disclaimer: This information is provided for research and educational purposes only. Applications should follow appropriate protocols and regulatory requirements. Not for diagnostic or therapeutic use.

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